McMillen B A, Scott S M, Davanzo E A
Department of Pharmacology, School of Medicine, East Carolina University, Greenville 27858.
J Pharm Pharmacol. 1988 Dec;40(12):885-7. doi: 10.1111/j.2042-7158.1988.tb06295.x.
The novel anxiolytic drug, buspirone, reverses catalepsy induced by haloperidol. A series of aryl-piperazine analogues of buspirone and other 5-hydroxytryptaminergic agonists were tested for their ability to reverse haloperidol induced catalepsy. Those drugs with strong affinity for 5-hydroxytryptamine1a receptors were able to reverse catalepsy. Drugs with affinity for other 5-HT receptors or weak affinity were ineffective. However, inhibition of postsynaptic 5-HT receptors neither inhibited nor potentiated reversal of catalepsy and leaves open the question as to the site or mechanism for this effect.
新型抗焦虑药物丁螺环酮可逆转氟哌啶醇所致的僵住症。对一系列丁螺环酮的芳基哌嗪类似物及其他5-羟色胺能激动剂逆转氟哌啶醇所致僵住症的能力进行了测试。那些对5-羟色胺1a受体具有强亲和力的药物能够逆转僵住症。对其他5-羟色胺受体具有亲和力或弱亲和力的药物则无效。然而,对突触后5-羟色胺受体的抑制既未抑制也未增强僵住症的逆转,这使得该效应的作用位点或机制问题悬而未决。